Boceprevir

Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6].

Product Specifications

CAS Number

[394730-60-0]

Product Name Alternative

EBP 520; SCH 503034

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

HCV; HCV Protease; SARS-CoV

Type

Reference compound

Related Pathways

Anti-infection; Metabolic Enzyme/Protease

Applications

COVID-19-anti-virus

Field of Research

Infection

Assay Protocol

https://www.medchemexpress.com/Boceprevir.html

Purity

99.0

Solubility

DMSO : 180 mg/mL (ultrasonic)

Smiles

O=C(N1[C@@H]([C@@]2([H])C(C)([C@]2(C1)[H])C)C(NC(C(C(N)=O)=O)CC3CCC3)=O)[C@@H](NC(NC(C)(C)C)=O)C(C)(C)C

Molecular Formula

C27H45N5O5

Molecular Weight

519.68

Precautions

H302, H315, H319, H335

References & Citations

[1]Njoroge FG, et al. Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection. Acc Chem Res. 2008 Jan;41 (1) :50-9.|[2]Yao M, et al. Conditional Inducible Triple-Transgenic Mouse Model for Rapid Real-Time Detection of HCV NS3/4A ProteaseActivity. PLoS One. 2016 Mar 4;11 (3) :e0150894.|[3]Coilly A, et al. Practical management of boceprevir and immunosuppressive therapy in liver transplant recipients with hepatitis C virus recurrence. Antimicrob Agents Chemother. 2012 Nov;56 (11) :5728-34.|[4]Berenguer M, et al. New developments in the management of hepatitis C virus infection: focus on boceprevir. Biologics. 2012;6:249-56.|[5]Burton MJ, et al. Telaprevir and boceprevir in african americans with genotype 1 chronic hepatitis C: implications for patients and providers. South Med J. 2012 Aug;105 (8) :431-6.|[6]Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6 (1) :212.